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48 Cards in this Set

  • Front
  • Back
decreased Km
increased affinity
Competitive inhibitor on 1/v;1/s graph
"competitively crosses" the uninhibited drug line at the y intercept; lesser affinity, same vmax
noncompetitive inhibitor on the 1/v;1/s graph
noncompetitor, noncrossing; shares x-intercept with uninhibited; same Km, lesser vmax
volume of distribution
amount of drug in the body/plasma drug concentration
clearance
rate of drug elimination/plasmadrug concentration

or

volume of distribution/elimination constant
half-life equation; drug infusion
(.7xVolume of distribution)/clearance

a drug infused at constant rate reaches 94% of steady state in 4 half lives
loading dose equation
=Cp x Vd/F (Cp is target plasma level and F is bioavailability)
Maintenance dose
=Cp x CL/F
Zero order elimination (give examples)
constant rate of elimination

PEA - Phanytoin, Ethanol, Aspirin PEAs are round like a Zero
First Order elimination
constant Fraction of drug is eliminated per unit time
effect of an antagonist
decreases potency, (more drug required for the same effect)
effect of a non-competitive antagonist
decreases efficacy (decreases the maximal effect possible by the agonist-drug)
partial agonists
have a LOWER MAXIMAL EFFECT/EFFICACY; may have a lower, higher or identicle potency (based on the EC50 of the full agonist).
Therapeutic index
TILE: TI = Ld50/Ed50 (toxic dose and effective doe respectively); safer drugs have a higher TI
G-protein linked second messengers.
KISS and KICK til you're SICK of SEX
QISS and QIQ til you're SIQ of SQS
Order: a1b1a2b2; m1m2m3; d1d2h1; h2v1v2
a1
q: vasoconstriction; pupil dilation
a2
i: decreases both sympathetic outflow and insulin release
b1
s: increases heart rate contractility, renin release, and lipolysis
b2
s: vaso/broncho dilation; increases HR contractility, lipolysis, glucagon release

decreases uterine tone
m1
q: CNS, enteric nervous system
m2
i: decreases HR and contractility
m3
q: increases exocrine secretion, gut peristalsis, bladder contraction, bronchoconstriction; increases pupillary sphincter tone (miosis) and ciliary contraction (accomodation
d1
s: relaxes renal vascular smooth muscle
d2
i: modulares transmitter release, esp. in the brain
h1
q: increases nasal and bronchial mucus, contraction of the bronchioles, pruritis, pain
h2
s: increases gastric acid secretion
v1
q: vascular smooth muscle contraction
v2
s: increases H2O permeability and reabsorption in the collecting tubules of the kidney
Gq receptor types
HAVe 1 M&M - H1, a1, V1, M1, M3
Gs receptor types
stimulated To(2) BeHaVe BaD1y - B2, H2, V2, B1, D1
Gi receptor Types:
MAD 2's: M2 a2 D2
Cholinergic syndromes
Over-stimulation of ACh receptors:

DUMBBELSS: diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skm/cns, lacrimation, sweating, salivation
treatment of Cholinergic syndrome
atropine (M antagonist) and pralidoxime (regenerates cholinesterase)
selective B2 agonists
MAST - metaprotenerol, albuterol, salmeterol, terbutaline
B1-antagonists
A BEAM of B1-blockers: Acebutolol, Betaxolol, Esmolol, Atenolol, Metoprolol
B1/B2 antagonists
Tim and Nadine Pin a Label on their Property: Timolol, Nadolol, Pindolol, Labetolol, Propranolol
Therapeutic Index
TILE: TI = LD50/ED50

increased TI = increased safety
zero order elimination
PEA: phenytoin Ethanol Aspirin

elimination decreases linearly with time
First order elimination
Fractional elimination with time causing an exponential decrease in [plasma]
P450 Inducers
Queen Barb was INDUCED to Steal Phen-phen and Refuse Greasy Carbs

Queen - quinidine
Barb - Barbiturates
Steals - St. Johns Wood
Phen-Phen (and) - Phenytoin
Refuses - Rifampin
Greasy - Greseofulvan
Carbs - Carbamazapine
P450 Inhibitors
Drink from a KEG and get SICk and INHIBITED

Ketoconazol
Erythromycin (macrolids except azithro)
Grapefruit juice
Sulfonamides
Isoniazid
Cimetidine
Drugs contraindicated in Pregnancy
SAFE Moms Take Really Good Care

Sulfonamides - kernicterus
Aminoglycosides - ototoxicity
Fluoroquinolones - cartilaginous damage
Erythromycin - acute cholestatis hepatitis in Mom and Clarithromycin is embryotoxic
Metronidazol - Mutagenesis
Tetracyclin - teeth colored and bone problems
Ribavirin - teratogen
Gresiofulvan - teratogen
Chloramphenical - Grey Baby Syndrome

Also warfarin
Bacteriostatic drugs
ECSTaTiC

Erythromycin
Clindamycin
Sulfamethoxazole
Trimethoprim
Tetracyclins
Chloramphenicol
Bacterocidal drugs
Very Finely Proficient At Cell Murder

Vancomycin
Fluoroquinolones
Penicillin
Aminoglycosides
Cephalosporine
Metronidazol
what is MAC
anesthetics: minimal alveolar concentration at which 50% of the population is anesthetized...it decreases with age.
how does MAC relate to potency
potency = 1/MAC

decreased MAC means increased potency and visa versa
Blood solubility relates to what?

give example of the relationship
induction and recovery.

decreased blood solubility = rapid induction and rapid recovery

increased blood solubility = slow induction and slow recovery
lipid solubility relates to what?

give an example of the relationship
potency and MAC

increased lipid solubility means increased potency and therefore decreased MAC.